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Systems Biology of Metabolic Regulation by Estrogen Receptor Signaling in Breast Cancer
10:36

Systems Biology of Metabolic Regulation by Estrogen Receptor Signaling in Breast Cancer

Published on: March 17, 2016

Selective estrogen receptor modulators (SERMs): mechanisms of anticarcinogenesis and drug resistance

Joan S Lewis1, V Craig Jordan

  • 1Fox Chase Cancer Center, Alfred G. Knudson Chair of Cancer Research, 333 Cottman Avenue, Philadelphia, PA 19111, USA.

Mutation Research
|August 9, 2005
PubMed

Insights

Selective estrogen receptor modulators (SERMs) offer tissue-specific estrogenic effects, crucial for breast cancer treatment and prevention by targeting estrogen receptors (ERs). Understanding SERM mechanisms combats resistance and improves therapeutic outcomes.

Area of Science:

  • Endocrinology
  • Oncology
  • Molecular Biology

Background:

  • Estrogens, particularly 17beta-estradiol (E2), play a dual role in women's health, influencing both beneficial effects and promoting breast cancer development.
  • Estrogenic responses are primarily mediated by estrogen receptors (ERs), ERalpha and ERbeta, which are ligand-dependent transcription factors.

Purpose of the Study:

  • To review the therapeutic applications of Selective Estrogen Receptor Modulators (SERMs) in medicine, with a focus on breast cancer treatment and prevention.
  • To elucidate the molecular mechanisms underlying the tissue-selective actions of SERMs.
  • To discuss the development of resistance to SERM therapy.

Main Methods:

  • Review of existing literature on SERMs, estrogen receptors, and breast cancer.
  • Analysis of molecular mechanisms involving ER conformational changes and interactions with coregulatory proteins.
  • Examination of factors influencing SERM biocharacter, including coactivator/corepressor expression and target gene promoters.

Main Results:

  • SERMs like Tamoxifen and Raloxifene demonstrate efficacy in breast cancer prevention and treatment by modulating ER activity.
  • Distinct ER ligand binding induces conformational changes, affecting interactions with coactivators and corepressors, leading to tissue-specific effects.
  • The efficacy of SERMs is influenced by the relative expression of coregulatory proteins and the specific ER and target gene promoter involved.

Conclusions:

  • SERMs are vital in managing ER-positive breast cancer, offering both therapeutic and preventive benefits.
  • Understanding the molecular basis of SERM action is key to optimizing their use and overcoming treatment resistance.
  • Continued research into SERM mechanisms is essential for advancing endocrine therapy in oncology.

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